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CAS No.: 311316-96-8

JMJD7-IN-1 Catalog No. CSN29559

Synonyms: JMJD7 inhibitor Cpd-3

JMJD7-IN-1 is a potent JMJD7 inhibitor with IC50 value of 6.62μM.

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描述JMJD5 and JMJD7 (JMJD5/7) are responsible for the clipping of arginine methylated histone tails to generate "tailless nucleosomes", which could release the pausing RNA polymerase II (Pol II) into productive transcription elongation. JMJD5/7 function as endopeptidases that cleave histone tails specifically adjacent to methylated arginine residues and continue to degrade N-terminal residues of histones via their aminopeptidase activity^[2]. Knockouts of JMJD5 and JMJD7 dramatically increase the content of arginine-methylated histone tails as well as the overall content of histone subunits in cells. Deletion of JMJD7 genes in human breast cancer cells drastically reduces their growth in soft agar^[3]. JMJD7 was present at gene promoters and its promoter occupancy changed upon osteoclast differentiation. Further, JMJD7 downregulation caused more rapid osteoclast differentiation^[4]. The JMJD7-PLA2G4B fusion protein does not encompass the full JmjC domain of JMJD7-predicting absence of any enzymatic activity - but consists of nearly the whole PLA2G4B protein, the functions of JMJD7-PLA2G4B are likely to match those of PLA2G4B. In the same vein, the association of a sequence variant of the JMJD7-PLA2G4B gene with high-risk autism is unlikely due to dysregulated JMJD7 enzymatic activity^[5]. JMJD7-IN-1 efficiently binds to JMJD7, with an IC50 of 3.80 μM. JMJD7-IN-1 (72 h) inhibits the growth of T-47d, SK-BR-3, Jurkat and Hela cells, with IC50s of 9.40 μM, 13.26 μM, 15.03 μM and 16.14 μM, respectively. JMJD7-IN-1 (0.1-1000 μM) dose-dependently inhibits the activity of JMJD7, with an IC50 of 6.62 μM^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7537 mL
- 13.7684 mL
- 27.5367 mL
- 5 mM
- 0.5507 mL
- 2.7537 mL
- 5.5073 mL
- 10 mM
- 0.2754 mL
- 1.3768 mL
- 2.7537 mL

技术信息

CAS号	311316-96-8	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C16H8Cl2N2O4	运输	蓝冰
分子量	363.15	别名	JMJD7 inhibitor Cpd-3

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